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Literature summary for 3.4.21.109 extracted from

  • Duchene, D.; Colombo, E.; Desilets, A.; Boudreault, P.L.; Leduc, R.; Marsault, E.; Najmanovich, R.
    Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptase and matriptase-2 (2014), J. Med. Chem., 57, 10198-10204.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
hepatocyte activation inhibitor 1 HAI-1, inhibition of matriptase Homo sapiens
KNAR more selective for matriptase compared to matriptase-2 Homo sapiens
LWWR 2-fold selectivity for matriptase-2 against matriptase Homo sapiens
additional information peptide inhibitor docking study with matriptase and matriptase-2, overview Homo sapiens
RLSR
-
Homo sapiens
RNPR more selective for matriptase compared to matriptase-2 Homo sapiens
WCYR more selective for matriptase compared to matriptase-2 Homo sapiens
WRER more selective for matriptase compared to matriptase-2 Homo sapiens
YKAR
-
Homo sapiens
YYVR 13times more selective for matriptase-2 than matriptase Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
proform matriptase + H2O Homo sapiens matriptase is expressed as a zymogen and is autocatalytically processed and activated through cleavage at Arg614 within the RQAR614-VVGG activation sequence mature matriptase
-
?
proform matriptase-2 + H2O Homo sapiens matriptase-2 is expressed as zymogen form and undergoes autocatalysis at Arg576 within the PSSR576-IVGG sequence located in the consensus activation site of its pro-domain mature matriptase
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8IU80
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification Matriptase is expressed in epithelial cells as a zymogen and needs to be activated. It undergoes spontaneous hydrolysis of a peptide bond at the Gly149 in the SEA domain. The protease is then autocatalytically processed and activated through cleavage at Arg614 within the RQAR614-VVGG activation sequence. Matriptase-2 is exclusively expressed in the liver initially under zymogen form. Matriptase-2 undergoes autocatalysis at Arg576 within the PSSR576-IVGG sequence located in the consensus activation site of its pro-domain Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
epithelial cell is expressed in epithelial cells as a zymogen Homo sapiens
-
liver matriptase-2 is exclusively expressed in the liver initially under zymogen form Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Boc-Gln-Ala-Arg-7-amido-4-methylcoumarin + H2O fluorogenic substrate Homo sapiens Boc-Gln-Ala-Arg + 7-amino-4-methylcoumarin
-
?
proform matriptase + H2O matriptase is expressed as a zymogen and is autocatalytically processed and activated through cleavage at Arg614 within the RQAR614-VVGG activation sequence Homo sapiens mature matriptase
-
?
proform matriptase-2 + H2O matriptase-2 is expressed as zymogen form and undergoes autocatalysis at Arg576 within the PSSR576-IVGG sequence located in the consensus activation site of its pro-domain Homo sapiens mature matriptase
-
?

Synonyms

Synonyms Comment Organism
matriptase-2
-
Homo sapiens

General Information

General Information Comment Organism
malfunction a mutation in matriptase is implicated in autosomal recessive ichtyosis withhypotrichosis a rare skin disease Homo sapiens
physiological function deregulation of matriptase can lead to various pathologies. Matriptase is thought to be implicated in osteoarthritis by initiating and inducting cartilage destruction Homo sapiens